Lung cancer is the major cause of human death in the world. Epidermal growth factor receptor (EGFR) is highly expressed in more than 60% of non-small cell lung cancer (NSCLC) patients. With the development of cancer therapeutic, more and more specific genetic mutations have been identified in NSCLC, for examples, EGFR, anaplastic lymphoma kinase (ALK), KRAS, ROS, and LKB1.
These were taken as molecular targets for individual comprehensive therapy for NSCLC patients. About 85% of EGFR mutations identified from patients are in-frame deletions in exon19 and the L858R point substitution in exon 21 of EGFR, which are biomarkers for good response to EGFR tyrosine kinase inhibitors (TKIs). Although it is an outstanding therapy for most patients with EGFR mutation, another new additional EGFR mutation such as T790M were identified, which eventually led to TKI resistance after one year. Therefore, it is urgently needed to discover more effective agents as candidate drugs for TKIs-resistant NSCLC patients.